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Spr24 Pharm II > Opioids Agonists (Exam II) > Flashcards

Opioids Agonists (Exam II) Flashcards

1
Q

What are opioids effects on the CO₂ medullary center?

A
  • Opioids inhibit the CO₂ medullary center.
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2
Q

Differentiate opioids from narcotics.

A
  • Opioids = all exogenous substances that bind to endogenous opioid receptors.
  • Narcotic = any substance that can produce dependence (stupor)
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3
Q

What two types of opioid chemical structures are there?

A
  • Phenanthrenes
  • Benzylisoquinolines
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4
Q

What types of drugs are Phenanthrenes?
What types of drugs are benzylisoquinolines?

A
  • Phenanthrenes: Morphine & codeine
  • Benzylisoquinoline: Papaverine
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5
Q

What is papaverine mostly used for?

A

Treating intra-arterial barbiturate administration (dilates the highly constricted artery).

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6
Q

What portions of the brain are the source of descending inhibitory signals?

A
  • Thalamus
  • PAG
  • Locus Coeruleus
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7
Q

What endogenous substances have the same effect as opioids?

A

Endorphins, Enkephalins, and Dynorphines.

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8
Q

Presynaptic inhibition of what neurotransmitters occurs with opioid administration?

A
  • ACh
  • Dopamine
  • NE
  • Substance P
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9
Q

How do opioids modulate pain at the cellular level?

A

At pre/postsynaptic opioid receptor sites in CNS
- ↑ K⁺ permeability (hyperpolarization)
- inactivate Ca⁺⁺ channel

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10
Q

Where are opioid receptors located in the brain?

A
  • PAG
  • Locus Coeruleus
  • RVM (rostral ventral medulla)
  • Hypothalamus
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11
Q

Where is the primary site of opioid receptors in the spinal cord?

A

Substantia gelatinosa (aka Laminae 2)

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12
Q

Where is/are opioid receptors found outside the CNS?

A
  • Sensory neurons & immune cells
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13
Q

What are the four (most important) types of opioid receptors?

A
  • Μu1 (μ₁)
  • Μu2 (μ₂)
  • Κappa (κ)
  • Delta (δ)
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14
Q

Which opioid receptor(s) is/are responsible for respiratory depression & physical dependence?

A
  • Μu2 and δ
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15
Q

Which receptors are responsible for constipation?

A
  • Μu2 primarily
  • δ (less)
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16
Q

Which receptors can cause urinary retention?
Are there any receptors that cause diuresis when bound?

A
  • Retention: Μu1 and δ
  • Diuresis: κ
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17
Q

All opioid receptors induce analgesia at both the brain and the spinal cord. T/F?

A
  • False. Μu2 receptors only cause analgesia at the spinal cord level.
18
Q

What opioid receptors have low abuse potential when bound?

A

Μu1 and κ

19
Q

Which opioid receptor is responsible for euphoria, bradycardia, hypothermia, and miosis when bound?

A

Mu1

20
Q

What agonists bind to each of the four opioid receptors?

A
  • Mu1 & Mu2 = endorphins, morphine, synthetics.
  • κ = dynorphins.
  • δ = enkephalins.
21
Q

Describe the adverse side effects of opioids on the cardiovascular system.

A
  • ↓BP from ↓SNS tone
  • ↓HR or histamine release = ↓BP
22
Q

What possible cardiovascular benefits do opioids provide?

A
  • Myocardial ischemia protection (decrease oxygen demand)
23
Q

What are the respiratory effects of opioids?
What would symptoms of overdose be?

A
  • Depressed CNS response to CO₂ causing a right shift of PaCO₂ (↑)
  • Overdose = apnea, miosis, coma.
24
Q

What drug would treat opioid ventilatory depression but not reverse analgesia?
How?

A
  • Physostigmine would by increasing CNS ACh levels.
25
Q

What would cause a leftward shift in PaO₂?
What would cause a rightward shift?

A
  • Leftward: Metabolic acidosis (to breathe off all that CO₂)
  • Rightward: sleep → opiates → anesthesia
26
Q

Why should caution be used when administering opioids to head trauma patients?

A
  • Opioids ↓CBF and possibly ICP
27
Q

What musculoskeletal abnormality occurs with opioid administration?
What makes this condition worse?
How is it treated?

A
  • Skeletal chest wall and abdominal muscle rigidity.
  • Mechanical ventilation
  • Muscle relaxants and/or naloxone
28
Q

What are sphincter of Oddi spasms?
Which drugs can cause this?

A
  • Biliary smooth muscle spasm
  • Fentanyl (99%), Morphine (53%), and Meperidine (61%). (Opioids)
29
Q

What drugs should be used for ERCP cases?

A
  • Non-opioids (multimodal approach w/ NSAIDs, gabapentin, etc.)
30
Q

How are opioid-induced sphincter of Oddi spasm’s treated?

A
  • Naloxone
  • Glucagon (2mg IV given incrementally) and causes no opioid antagonism.
31
Q

How long does it take (generally) to develop tolerance to opioids?
What causes tolerance?

A
  • 2-3 weeks
  • Downregulation (desensitized and decreased number of opioid receptor)
32
Q

What is the dosage of morphine?
When does it peak?
How long does it last?

A
  • 1 - 10 mg IV
  • Peak: 15 - 30 minutes
  • Duration: 4-5 hours
33
Q

How is morphine metabolized?
What is the active metabolite and its significance?

A
  • Glucuronidation in the liver.
  • Morphine-6-glucuronide = comprises only 5-25% of morphine metabolites but is an active anaglesic causing late resp depression.
34
Q

What would occur with morphine overdose in a renal failure patient?

A
  • Prolonged ventilatory depression.
35
Q

What receptors does meperidine agonize?

A
  • μ and κ receptors
  • α2 receptors as well
36
Q

What are the analogues of meperidine?
What other drugs does meperidine have a similar organic structure to?

A
  • Fentanyl & it’s derivatives
  • Lidocaine & Atropine
37
Q

How potent is Meperidine? (comp)
How long does it last?

A
  • 10% as potent as morphine
  • Duration: 2-4 hours
38
Q

What is the primary indication for meperidine?
What dose is used?

A
  • Post-operative shivering
  • 12.5mg IV
39
Q

When should meperidine not be used?

A
  • Bronchoscopies (promotes coughing)
40
Q

How potent is fentanyl?

A
  • 75 - 125 x morphine.

Spr24 Pharm II (32 decks)

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